公开(公告)号：US10745383B2

公开(公告)日：2020-08-18

申请号：US15748795

申请日：2016-07-29

申请人： CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD. ,  LIANYUNGANG RUNZHONG PHARMACEUTICAL CO., LTD. ,  CENTAURUS BIOPHARMA CO., LTD.

发明人： Na Zhao ,  Shulong Wang ,  Xijie Liu ,  Yuandong Hu ,  Hui Zhang ,  Hong Luo ,  Yong Peng ,  Yongxin Han ,  Xiquan Zhang ,  Hongjiang Xu

IPC分类号： C07D401/14 ,  C07D401/04 ,  C07D401/12 ,  A61P35/00 ,  A61K31/53 ,  C07D251/26 ,  C07D251/18

摘要： Disclosed are compounds having formulae I and II or pharmaceutically acceptable salts or hydrates thereof, a preparation method thereof and pharmaceutical compositions thereof. The compounds having formulae I and II possesses an isocitrate dehydrogenase 2 (IDH2) inhibitory activity and are capable of treating IDH2 mutation-induced cancers.

公开(公告)号：US10654826B2

公开(公告)日：2020-05-19

申请号：US15748795

申请日：2016-07-29

申请人： CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD. ,  LIANYUNGANG RUNZHONG PHARMACEUTICAL CO., LTD. ,  CENTAURUS BIOPHARMA CO., LTD.

发明人： Na Zhao ,  Shulong Wang ,  Xijie Liu ,  Yuandong Hu ,  Hui Zhang ,  Hong Luo ,  Yong Peng ,  Yongxin Han ,  Xiquan Zhang ,  Hongjiang Xu

IPC分类号： C07D401/14 ,  C07D401/04 ,  C07D401/12 ,  A61P35/00 ,  A61K31/53 ,  C07D251/18 ,  C07D251/26

摘要： Disclosed are compounds having formulae I and II or pharmaceutically acceptable salts or hydrates thereof, a preparation method thereof and pharmaceutical compositions thereof. The compounds having formulae I and II possesses an isocitrate dehydrogenase 2 (IDH2) inhibitory activity and are capable of treating IDH2 mutation-induced cancers.

公开(公告)号：US10220037B2

公开(公告)日：2019-03-05

申请号：US15612030

申请日：2017-06-02

申请人： Pfizer Inc.

发明人： John Howard Tatlock ,  Indrawan James McAlpine ,  Michelle Bich Tran-Dube ,  Eugene Yuanjin Rui ,  Martin James Wythes ,  Robert Arnold Kumpf ,  Michele Ann McTigue ,  Ryan Patman

IPC分类号： C07D487/04 ,  A61K31/519 ,  C07D519/00 ,  A61K31/137 ,  A61K31/53 ,  C07D237/22 ,  C07D251/16 ,  C07D471/06 ,  C07D239/42 ,  C07D239/84 ,  C07D251/18 ,  C07D491/048 ,  A61P35/00 ,  A61P35/02 ,  A61P35/04 ,  A61K31/02 ,  C07C255/34

摘要： Compounds of the general formula): processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds.

公开(公告)号：US20180008561A1

公开(公告)日：2018-01-11

申请号：US15712026

申请日：2017-09-21

申请人： ELCELYX THERAPEUTICS, INC.

发明人： Alain D. BARON ,  Mark S. FINEMAN ,  Nigel R. A. BEELEY

IPC分类号： A61K31/155 ,  A61K9/00 ,  C07D307/52 ,  C07D255/02 ,  C07D251/18 ,  C07D251/10 ,  C07D249/14 ,  A61K45/06 ,  A61K31/55 ,  A61K31/53 ,  A61K31/4196 ,  A61K31/36 ,  A61K9/28 ,  A61K9/20 ,  C07D317/58 ,  C07D405/12

CPC分类号： A61K31/155 ,  A61K9/0053 ,  A61K9/2054 ,  A61K9/2813 ,  A61K9/282 ,  A61K9/2846 ,  A61K9/2866 ,  A61K31/36 ,  A61K31/4196 ,  A61K31/53 ,  A61K31/55 ,  A61K45/06 ,  C07D249/14 ,  C07D251/10 ,  C07D251/18 ,  C07D255/02 ,  C07D307/52 ,  C07D317/58 ,  C07D405/12 ,  A61K2300/00

摘要： Methods for improving the gastrointestinal tolerability of biguanide compounds and for treating metabolic disorders and/or inducing weight loss in patients in need thereof, particularly in individuals having a contraindication for treatment with biguanide compounds, are provided comprising administering delayed release formulations of such biguanide compounds, including metformin, targeted to the small intestine.

公开(公告)号：US20170348318A1

公开(公告)日：2017-12-07

申请号：US15630886

申请日：2017-06-22

申请人： Agios Pharmaceuticals, Inc.

发明人： Jeremy Travins ,  Luke Utley

IPC分类号： A61K31/53 ,  C07D417/12 ,  C07D413/12 ,  C07D403/12 ,  C07D403/04 ,  C07D401/14 ,  C07D401/12 ,  C07D401/04 ,  C07D251/18 ,  C07D417/14 ,  A61K45/06

CPC分类号： A61K31/53 ,  A61K45/06 ,  C07D251/18 ,  C07D251/48 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

摘要： Provided are compounds of formula (I), Wherein: ring A and ring B are each independently an optionally substituted 5-6 membered monocyclic aryl or heteroaryl. The compounds are inhibitors of isocitrate dehydrogenase 2 (IDH2) mutants useful for treating cancer.

公开(公告)号：US09822105B2

公开(公告)日：2017-11-21

申请号：US15305823

申请日：2015-04-22

申请人： BASF SE

发明人： Julia Major ,  Florian Vogt ,  Frederick Calo ,  Thomas Seitz ,  Doreen Schachtschabel ,  Trevor William Newton ,  Kristin Hanzlik ,  Johannes Hutzler ,  Klaus Kreuz ,  Stefan Tresch

IPC分类号： C07D413/12 ,  C07D405/12 ,  A01N43/68 ,  C07D405/14 ,  C07D251/18 ,  A01N43/76

CPC分类号： C07D413/12 ,  A01N43/68 ,  A01N43/76 ,  C07D251/18 ,  C07D405/12 ,  C07D405/14

摘要： The present invention relates to diaminotriazine compounds and to their use as herbicides. The present invention also relates to agrochemical compositions for crop protection and to a method for controlling unwanted vegetation. wherein A is a fused saturated or unsaturated, 5-, 6-membered carbocycle or a fused saturated or unsaturated, 5-, 6-membered heterocycle; P is 1 or 2 q is 0, 1, 2 or 3; Rb is inter alia halogen, OH, CN, amino, NO2, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C1-C6-alkoxy, C2-C6-alkenyloxy, C2-C6-alkynyloxy, etc.; R1 is inter alia H, OH, S(O)2NH2, CN, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, (C3-C6-cycloalkyl)-C1-C4-alkyl, C1-C6-alkoxy, etc.; R2 is inter alia H, OH, S(O)2NH2, CN, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, (C3-C6-cycloalkyl)-C1-C4-alkyl, C1-C6-alkoxy, etc; X is a radical selected from the group consisting of CR3R4R5 phenyl, which is unsubstituted or carries 1, 2, 3, 4 or 5 radicals RAr; NR3aR3b, OR3c, S(O)kR3d, k being 1, 2 or 3, and including their agriculturally acceptable salts.

公开(公告)号：US09718788B2

公开(公告)日：2017-08-01

申请号：US15249851

申请日：2016-08-29

申请人： MILLENNIUM PHARMACEUTICALS, INC.

发明人： Christopher F. Claiborne ,  Stephen Critchley ,  Steven P. Langston ,  Hirotake Mizutani ,  Edward J. Olhava ,  Stephane Peluso ,  Irache Visiers ,  Stepan Vyskocil

IPC分类号： C07D213/82 ,  C07D239/48 ,  C07D487/04 ,  C07D239/42 ,  C07D213/56 ,  C07D213/69 ,  C07D401/04 ,  C07D403/04 ,  C07D471/04 ,  C07D471/08 ,  C07D473/34 ,  C07D473/30 ,  A61K31/53 ,  C07D251/18 ,  C07D251/48 ,  C07D213/74 ,  C07D401/06 ,  C07D213/81 ,  C07D239/36

CPC分类号： C07D239/42 ,  A61K31/53 ,  C07D213/56 ,  C07D213/69 ,  C07D213/74 ,  C07D213/81 ,  C07D213/82 ,  C07D239/36 ,  C07D239/48 ,  C07D251/18 ,  C07D251/48 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D471/04 ,  C07D471/08 ,  C07D473/30 ,  C07D473/34 ,  C07D487/04

摘要： This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.

公开(公告)号：US20170073331A1

公开(公告)日：2017-03-16

申请号：US15304798

申请日：2015-04-17

申请人： IMMUNOMET THERAPEUTICS INC.

发明人： Sung Wuk Kim ,  Hong Woo Kim ,  Sang Hee Yoo ,  Ji Sun Lee ,  Hye Jin Heo ,  Hong Bum Lee ,  Ji Ae Kook ,  Young Woo Lee ,  Mi Jeong Kim ,  Woong Cho

IPC分类号： C07D403/12 ,  C07C311/47 ,  C07D295/13 ,  C07D211/14 ,  C07D319/18 ,  C07D333/20 ,  C07D251/18 ,  C07D249/14 ,  C07D211/54 ,  C07C279/04 ,  C07C279/08 ,  C07D209/44 ,  C07C279/16 ,  C07C279/06 ,  C07D233/91 ,  C07D213/38 ,  C07C279/12 ,  C07D239/42 ,  C07C279/24 ,  C07D207/16 ,  C07D277/46 ,  C07D263/48 ,  C07C279/26

CPC分类号： C07D403/12 ,  C07C279/04 ,  C07C279/06 ,  C07C279/08 ,  C07C279/12 ,  C07C279/16 ,  C07C279/24 ,  C07C279/26 ,  C07C311/47 ,  C07C311/49 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/08 ,  C07C2602/10 ,  C07C2603/74 ,  C07D207/16 ,  C07D209/40 ,  C07D209/44 ,  C07D211/14 ,  C07D211/54 ,  C07D213/38 ,  C07D213/40 ,  C07D233/88 ,  C07D233/91 ,  C07D239/42 ,  C07D249/14 ,  C07D251/18 ,  C07D251/48 ,  C07D263/48 ,  C07D277/46 ,  C07D295/13 ,  C07D317/58 ,  C07D319/18 ,  C07D333/16 ,  C07D333/20

摘要： The present invention relates to guanidine compounds for inhibiting mitochondrial oxidative phosphorylation (OXPHOS) and use thereof. More specifically, the present invention relates to a pharmaceutical composition for preventing or treating a OXPHOS-related disease, particularly cancer, by inhibiting mitochondrial oxidative phosphorylation and reprogramming cellular metabolism.

摘要翻译： 本发明涉及用于抑制线粒体氧化磷酸化（OXPHOS）的胍化合物及其应用。 更具体地，本发明涉及通过抑制线粒体氧化磷酸化和重新编程细胞代谢来预防或治疗OXPHOS相关疾病，特别是癌症的药物组合物。

公开(公告)号：US20170044114A1

公开(公告)日：2017-02-16

申请号：US15305827

申请日：2015-04-22

申请人： BASF SE

发明人： Julia MAJOR ,  Florian VOGT ,  Frederick CALO ,  Thomas SEITZ ,  Doreen SCHACHTSCHABEL ,  Trevor William NEWTON ,  Kristin HANZLIK ,  Johannes HUTZLER ,  Klaus KREUZ ,  Stefan TRESCH ,  Mihiret Tekeste SISAY

IPC分类号： C07D251/18 ,  A01N43/68

CPC分类号： C07D251/18 ,  A01N43/68 ,  C07D251/48

摘要： The present invention relates to diaminotriazine compounds and to their use as herbicides. It also relates to agrochemical compositions for crop protection and to a method for controlling unwanted vegetation. wherein p is 1 or 2; q is 0, 1, 2 or 3 provided that p+q is 1, 2, 3 or 4; Q is inter alia a chemical bond, O, S(O)m, CRq1Rq2, NRq3, C(O), C(O)O, Ar is phenyl, which is unsubstituted or carries 1, 2, 3, 4 or 5 radicals RA Ra is inter alia hydrogen, halogen, OH, CN, amino, NO2, C1-C6-alkyl, etc; Rb is inter alia halogen, OH, CN, amino, NO2, C1-C6-alkyl, etc.; R1 and R2 are inter alia H, OH, S(O)2NH2, ON, C1-C6-alkyl, etc; X is a radical selected from the group consisting of CR3R4R5, phenyl, which is unsubstituted or carries 1, 2, 3, 4 or 5 radicals RAr; NR3aR3b, OR3c, S(O)kR3d, k being 1, 2 or 3; and including their agriculturally acceptable salts.

摘要翻译： 本发明涉及二氨基三嗪化合物及其作为除草剂的用途。 它还涉及用于作物保护的农用化学组合物和用于防治不需要的植物的方法。 式（I）其中p为1或2; q为0,1,2或3，条件是p + q为1,2,3或4; Q特别是化学键，O，S（O）m，CRq1 Rq2，NRq3，C（O），C（O）O，Ar是苯基，其未被取代或携带1,2,3,4或5 基团RA，R a尤其是氢，卤素，OH，CN，氨基，NO 2，C 1 -C 6 - 烷基等; Rb特别是卤素，OH，CN，氨基，NO 2，C 1 -C 6 - 烷基等; R1和R2特别是H，OH，S（O）2 NH 2，CN，C 1 -C 6烷基等; X是选自CR 3 R 4 R 5，苯基的基团，其为未取代的或带有1,2,3,4或5个基团RAr; NR3aR3b，OR3c，S（O）kR3d，k为1,2或3; 并包括其农业上可接受的盐。

公开(公告)号：US20150183753A1

公开(公告)日：2015-07-02

申请号：US14480513

申请日：2014-09-08

申请人： MILLENNIUM PHARMACEUTICALS, INC.

发明人： Christopher F. Claiborne ,  Stephen Critchley ,  Courtney Cullis ,  Steven P. Langston ,  Hirotake Mizutani ,  Edward J. Olhava ,  Stephane Peluso ,  Irache Visiers ,  Stepan Vyskocil ,  Gabriel S. Weatherhead

IPC分类号： C07D251/18

CPC分类号： C07D239/42 ,  A61K31/53 ,  C07D213/56 ,  C07D213/69 ,  C07D213/74 ,  C07D213/81 ,  C07D213/82 ,  C07D239/36 ,  C07D239/48 ,  C07D251/18 ,  C07D251/48 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D471/04 ,  C07D471/08 ,  C07D473/30 ,  C07D473/34 ,  C07D487/04

摘要： This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.

摘要翻译： 本发明涉及抑制E1活化酶的化合物，包含该化合物的药物组合物和使用该化合物的方法。 该化合物可用于治疗疾病，特别是细胞增殖病症，包括癌症，炎症和神经变性疾病; 和与感染和恶病质相关的炎症。